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• W1546592010 abstract "Epibatidine, a potent nicotinic agonist, was used to study the regional distribution of nicotinic acetylcholine receptor binding sites in the human brain. Saturation studies performed in the human temporal cortex with (±)-[3H]epibatidine revealed binding to two binding sites with Kd and Bmax values of 0.018 and 4.2 nM, 12.7 and 15.4 fmol/mg protein, respectively. Competition studies with (±)-[3H]epibatidine/unlabelled nicotine or [3H]nicotine/unlabelled (±)-epibatidine showed binding to two binding sites in the human temporal cortex (Ki=0.16 and 12.6 nM; 0.007 and 0.3 nM, respectively). Similarly, when unlabelled nicotine was used to displace (±)-[3H]epibatidine, two binding sites were also revealed in the thalamus and the cerebellum of human brain (Ki=0.065 and 7.7 nM; 0.07 and 12.5 nM, respectively). The regional binding of (±)−[3H]epibatidine binding in human brain was somewhat different from that of [3H]nicotine. A proportionally higher binding was observed for (±)-[3H]epibatidine in the cerebellum and the thalamus compared to [3H]nicotine, probably reflecting different selectivity to nicotinic receptor subtypes. A marked significant age-related decrease in (±)-[3H]epibatidine binding was observed in the frontal and the temporal cortices (−79%, −84%, respectively) of human subjects between 56–85 years of age, which was similar to that of [3H]nicotine (−82%, −79%, respectively). The (±)-[3H]epibatidine binding in the cerebellum decreased significantly with age (−77%), while [3H]nicotine binding showed no significant age-related changes in this brain region. The findings indicate that a specifically modulate regional nicotinic receptors in human brain." @default.
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• W1546592010 date "1998-08-01" @default.
• W1546592010 modified "2023-09-30" @default.
• W1546592010 title "Regional distribution of subtypes of nicotinic receptors in human brain and effect of aging studied by (±)-[]" @default.
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• W1546592010 doi "https://doi.org/10.1016/s0006-8993(98)00558-7" @default.
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